NAMPT inhibitor-linker 2

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CAS NO:

2241014-82-2

NAMPT inhibitor-linker 2 为ADC的一部分，由一种NAMPT的抑制剂作为有效载荷和一个连接物组成。ADC-4 由一个 NAMPT inhibitor-linker 2 和一个 anti-c-Kit 单克隆抗体组成，对表达 c-Kit 的细胞具有抑制作用，比如 GIST-T1 和 NCI-H526 细胞，IC₅₀值分别为<7 pM 和 40 pM。

生物活性

NAMPTinhibitor-linker 2 is a drug-linker conjugates forADC, composed of anNAMPTinhibitor as a payload, and a linker. ADC-4 consists of anNAMPTinhibitor-linker 2 and an anti-c-Kit monoclonal antibody, exihibits potent activity againstc-Kitexpressing cell lines such as GIST-T1 and NCI-H526, withIC₅₀s of<7 pM and 40 pM, respectively.

IC₅₀& Target

Traditional Cytotoxic Agents

体外研究
(In Vitro)

ADC-4 exihibits potent activity against c-Kit expressing cell lines such as GIST-T1 and NCI-H526, with IC₅₀s of<7 pm and 40 pm, respectively^[1].
ADC-4 (0.01 nM-10 nM, 144 hours) inhibits cell proliferation of GIST-T1 cells, but does not affect the cell cycle^[1].

Cell Proliferation Assay^[1]

Cell Line:	GIST-T1 cells
Concentration:	0.1 pM-10 nM
Incubation Time:	144 hours
Result:	Inhibited the cell proliferation of GIST-T1 cells at 0.01-10 nM, and the inhibition remained unchanged after 1 nM.

体内研究
(In Vivo)

ADC-4 (20 mg/kg, i.v. for 28 days) is tolerated, and causes tumor stasis in mice bearing GIST-T1 cells^[1].

Animal Model:	Female scid-beige (SCID bg) mice^[1]
Dosage:	20 mg/kg
Administration:	A single intravenous injection (i.v.) for 28 days
Result:	Significantly inhibited the growth of tumor in mice.

分子量

624.66

Formula

C₃₄H₃₃FN₆O₅

CAS 号

2241014-82-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.